It is well established that acne is associated with sebum production and that androgens stimulate sebum production whereas estrogens suppress sebum production, estrogen therapy being indicated as a possible means of treating acne. Several reports indicate that oral contraceptives or the individual active estrogenic components thereof, for example, ethinyl estradiol and derivatives are useful in treating acne in both males and females. In recent years it has become apparent that estrogenic products currently in use possess certain undesirable side effects which must be set against the undoubted benefits resulting from their use. The use of estrogens for the treatment of acne in women can lead to uterine bleeding and spotting and breast tenderness. In men estrogen administration can have a feminizing effect and may result in gynecomastia and impotence (L. F. Goodman and A. Gilman, The Pharmacological Basis of Therapeutics, 4th Ed., The MacMillan Company, p. 1547 (1970)). Estrogenic therapy has been reported to give rise to other deleterious side effects. For example, diethylstilbestrol, a once widely used and well established estrogen has been implicated as possibly being responsible for vaginal cancer and adenosis in the female offspring of pregnant women treated with the the compound (Lancet 1975, 1960). Also, ethinyl estradiol and mestranol, which represent estrogenic compounds in current oral contraceptives, are now known to be involved in certain serious side effects associated with oral contraceptives including depression (Nature 243, 58 (1973)), hypertension (Am. J. Obstet. Gynecol. 112, 912 (1972)), carbohydrate and lipid abnormalities (Lancet 1969, October 11, p. 783), interference with blood clotting mechanism resulting in thrombosis and stroke (Ann. Intern. Med. 72, 111 (1970)), and jaundice (Am. J. Obstet. Gynecol. 119, 165 (1974)). Consequently, there is a need for an improved method of treating acne.
The present invention provides a novel and improved method of treating acne which comprises administering androstene compounds described more fully hereinbelow. Some of the compounds employed in this invention, for example, 19-hydroxyandrost-4-ene-3,17-dione and the 19-oxo derivative thereof have been involved in numerous in vitro studies wherein their role in the metabolism of androgen has been investigated. Additionally, 19-hydroxyandrost-4-ene-3,17-dione is reported to have been administered to two healthy male subjects each twenty-one years of age (J. Clin. Endocrinol. Metab. 28, 1401 (1968)). To applicants' knowledge the use of the compounds employed in the present invention in the treatment of acne has not been taught or suggested heretofore.
Also, 3-oxo-17.beta.-hydroxyandrost-4-en-19-al has been reported in U.S. Pat. Nos. 3,235,573, issued Feb. 15, 1966, and 3,449,381, issued June 10, 1969 wherein the utilities disclosed are anabolic-androgenic activity, inhibition of pituitary gonadotrophins and adrenocorticotrophin, antiestrogenic, blood, liver and adrenal cholesterol lowering properties, control of fertility and psychotic conditions, and appetite stimulants.